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Table 2 The binding affinities of toxin BmKKx2 towards wild-type and mutant hERG channel

From: Open conformation of hERG channel turrets revealed by a specific scorpion toxin BmKKx2

hERG mutant IC50a nb IC50(mut)/IC50(wt)
  nM   
Wild Type 6.7 ± 1.7 7 1.0
H578A N.Ec 5 -e
D580A L.Ed 5 -
R582A 76.5 ± 32.6 4 11.4
I583A 87.5 ± 16.8 4 13.1
W585A N.E 6 -
L586A 24.3 ± 8.4 4 3.6
H587A 59.7 ± 31.7 5 8.9
N588A 14.5 ± 4.3 4 2.2
L589A L.E 6 -
D591A 19.6 ± 1.7 4 2.9
Q592A 89.5 ± 39.8 5 13.4
K595A 65.2 ± 19.1 5 9.7
P596A 60.8 ± 23.4 4 9.1
Y597A 118.2 ± 26.7 4 17.6
N598A 15.2 ± 4.8 4 2.3
S600A 12.1 ± 3.5 4 1.8
K608A 116.1 ± 29.2 5 17.3
D609A L.E. 8 -
K610A 6.7 ± 5.1 5 1.0
T613A 42.6 ± 17.1 5 6.4
N629A L.E 7 -
S631A 698.0 ± 64.4 5 104.2
  1. aIC50 value(half-maximum inhibition concentration) represents as Mean ± Standard Error.
  2. bnumber of independent experiments.
  3. cno expression, can’t detect fluorescent flag in all transfected HEK 293 T cells.
  4. dlow expression, with detectable fluorescent flag but can only elicit weak current in all transfected HEK 293 cells.
  5. e- means the lack of IC50 value of mutants.